An overview of conjugates of coordination complexes and organometallic complexes of Pt, Ru, Fe, Re, lanthanoids and other metals with natural and synthetic estrogens and antiestrogens targeting the nuclear estrogen receptors is provided. These conjugates are used as targeted cytotoxic agents or - if radiolabeled - as imaging probes for the detection of estrogen receptor-rich tissues such as hormone-dependent tumours. They are assessed with respect to their estrogen receptor binding affinities, potential synergistic cytotoxic effects in cancer cells and their specificity for tumour over non-malignant cells and tissues. The mechanisms of their modes of action are discussed. Pertinent literature is covered up to 2008.